Research Papers:

Doxorubicin-triggered self-assembly of native amphiphilic peptides into spherical nanoparticles

Xiaobo Fan, Fengfeng Zhao, Xiyong Wang and Guoqiu Wu _

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Oncotarget. 2016; 7:58445-58458. https://doi.org/10.18632/oncotarget.11213

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Xiaobo Fan1,2,*, Fengfeng Zhao2,*, Xiyong Wang2, Guoqiu Wu1,2

1Center of Clinical Laboratory Medicine of Zhongda Hospital, Southeast University, Nanjing, 210009, China

2Medical School, Southeast University, Nanjing, 210009, China

*These authors have contributed equally to this work

Correspondence to:

Guoqiu Wu, email: [email protected]

Keywords: matrilin-1 C-terminal peptide, self-assembly, nanosphere, drug delivery, cancer therapy

Received: May 16, 2016    Accepted: July 19, 2016    Published: August 11, 2016


In this study, we designed and fabricated self-assembly nanospheres, which consisted of a P45 peptide and doxorubicin (Dox). P45 is a hybrid peptide composed of an Arg-Gly-Asp motif linked to the human matrilin-1 C-terminal domain by a serine linker. The fabricated nanospheres had a uniform mulberry-like spherical shape, a diameter of 63 nm, excellent polydispersity, and high Dox drug-loading efficiency. In the presence of the RGD motif, the Dox/P45 nanospheres could specifically target A549 cells, which have high integrin αvβ3 expression. Confocal laser scanning microscopy and flow cytometry results showed the enhanced cellular uptake of Dox/P45, and the CCK8 assay indicated the low cytotoxicity of the nanospheres to normal human embryonic kidney 293 cells. Furthermore, the fabricated nanospheres were stable in a physiological environment, but they disassembled and exhibited a rapid Dox release in an acidic atmosphere, allowing for a specific pH-sensitive release into cytosol after cellular uptake. These results suggest that natural amphiphilic peptides can be used as carriers of nanodrugs for targeting delivery as well as controlled drug release for cancer therapy.

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